Field of the Disclosure
The present disclosure relates to novel crystalline forms of dolutegravir sodium and a process for the preparation thereof.
Description of the Related Art
Dolutegravir (DTG, GSK1349572) is an integrase inhibitor being developed for the treatment of human immunodeficiency virus (HIV)-1 infection.
TIVICAY® tablets contain dolutegravir sodium, which is an HIV-1 integrase strand transfer inhibitor (INSTI). Dolutegravir sodium is chemically known as sodium (4R, 12aS)-9-((2,4-difluorobenzyl)carbamoyl)-4-methyl-6, 8-dioxo-3, 4, 6, 8, 12, 12a-hexahydro-2H-pyrido[1′,2′:4,5]pyrazino[2, 1-b][1,3]oxazin-7-olate, having the structure below:

PCT Publication No. WO2010068253A1 (which is hereby incorporated by reference) discloses a crystalline form of dolutegravir sodium characterized by the following powder X-ray diffraction (PXRD) pattern having peaks at 6.4, 9.2, 13.8, 19.2 and 21.8±0.2° 2θ; and a crystalline form of dolutegravir sodium hydrate characterized by the following diffraction peaks in the PXRD pattern at 8.0, 9.3, 11.3, 16.0 and 22.8±0.2° 2θ.
PCT Publication No. WO2013038407A1 (which is hereby incorporated by reference) discloses amorphous dolutegravir sodium characterized by the following characteristic peaks in infrared absorption spectrum at about 662±4, 766±4, 851±4, 886±4, 959±4, 1025±4, 1055±4, 1090±4, 1133±4, 1206±4, 1233±4, 1248±4, 1279±4, 1318±4, 1356±4, 2325±4 and 2348±4 cm−1.
The present disclosure provides novel crystalline forms of dolutegravir sodium.